Home Tools

E6201

Catalog No. T61755 CAS 603987-35-5

E6201 (ER-806201) is a potent dual kinase inhibitor targeting MEK1 and FLT3, inhibiting their activities in an ATP-competitive manner. It effectively suppresses MEK1-induced ERK2 phosphorylation (IC50 = 5.2 nM), MKK4-induced JNK phosphorylation (IC50 = 91 nM), and MKK6-induced p38 MAPK phosphorylation (IC50 = 19 nM). E6201 exhibits anti-tumor and anti-psoriasis effects [1] [2].

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

E6201, CAS 603987-35-5

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 1,520.00
50 mg	10-14 weeks	$ 1,980.00
100 mg	10-14 weeks	$ 2,500.00

Bulk Inquiry

This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	E6201 (ER-806201) is a potent dual kinase inhibitor targeting MEK1 and FLT3, inhibiting their activities in an ATP-competitive manner. It effectively suppresses MEK1-induced ERK2 phosphorylation (IC50 = 5.2 nM), MKK4-induced JNK phosphorylation (IC50 = 91 nM), and MKK6-induced p38 MAPK phosphorylation (IC50 = 19 nM). E6201 exhibits anti-tumor and anti-psoriasis effects [1] [2].
In vitro	E6201 is distinguished as an inhibitor explicitly targeting the MEKK1 and MEK families, without impacting the MAPK family members, demonstrating selective inhibitory effects on MEKK1-induced phosphorylation of MEK1, MKK4, and MKK6 (IC50 values: 31, 522, and 65 nM, respectively). Notably, at a concentration of 10 μM, E6201 does not influence other proteins in the MAPK family such as ERK2, JNKs, and p38 MAPK. Its capability extends to thwarting LPS-induced TNF transcription (IC50: 50±14 nM) while barely affecting β-actin transcription up to concentrations of 3 μM. E6201 also shows inhibitory actions on specific receptor tyrosine kinases—including VEGFR2, PDGFR, the hepatocyte growth factor receptor, and EGFR (IC50 values: 350, 860, 1100, and 5400 nM, respectively)—and the nonreceptor tyrosine kinase Syk (IC50: 460 nM), while sparing ZAP-70, IKK, and PKC activity even at elevated concentrations of 10 μM and 100 μM, respectively. This compound further inhibits IL-2 production post-PHA-P activation (IC50: 18 nM), curtails proliferation of EGF-stimulated human keratinocytes (IC50: 160 nM), and suppresses IL-8 production in keratinocytes post-IL-1α or TNFα stimulation (IC50 values: 60 and 30 nM, respectively). Additionally, E6201 effectively inhibits production of TNFα, IL-1, IL-6, and IL-8 in human PBMCs (IC50 values: 20, 16, 52, and 53 nM, respectively), showcases potent inhibition of triple-negative breast cancer (TNBC) cell proliferation and colony formation in a dose-dependent manner, induces G1 phase cell cycle arrest, and triggers apoptosis in TNBC cells at 1 μM, substantiated by a significant reduction in phospho-ERK expression levels and sustained effects observed through Western Blot Analysis.
In vivo	Administering E6201 (30 mg/kg; via tail vein injection three times per week) demonstrated prominent inhibition of TNBC xenograft tumor growth and significantly reduced pERK and Ki-67 expression in xenograft tumor tissues [2]. The study utilized female Nod.Scid gamma mice, aged 4 to 6 weeks, implanted with MDA-MB-231-LM2 xenograft tumors [2]. Over a period of 17 days, the dosage and method of administration remained consistent. Compared to mice receiving a vehicle control, those treated with E6201 exhibited a 60% suppression in tumor growth.

Molecular Weight	389.44
Formula	C21H27NO6
CAS No.	603987-35-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

E6201 603987-35-5 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.